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Zaleplon double-release capsule and preparation method thereof

A zaleplon, double-release technology, applied in the field of zaleplon double-release capsule preparation and its preparation, can solve the problem of high blood drug concentration

Inactive Publication Date: 2012-12-19
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the high fat solubility and plasma protein binding rate of zaleplon, the release of common preparations is too fast, resulting in high blood concentration and inducing side effects (such as headache, drowsiness, dizziness, nausea and vomiting, fatigue, memory difficulties, dreaminess, etc.) and other adverse reactions) the probability of increased

Method used

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  • Zaleplon double-release capsule and preparation method thereof
  • Zaleplon double-release capsule and preparation method thereof
  • Zaleplon double-release capsule and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0088] Zaleplon double-release capsules of the present invention comprise quick-release pellets and delayed-release pellets, and the weight percentages of the quick-release pellets and delayed-release pellets are respectively 40% and 60%, i.e. immediate release The mass ratio between the pellets and the delayed-release pellets is 2:3;

[0089] With respect to the immediate-release part in the zaleplon double-release capsules, the quick-release pellets are made up of the following raw materials in percentage by weight: zaleplon 16.1%, sucrose pellets 36.6%, filler mannitol 14.1% , binder hypromellose 8.1%, disintegrant A crospovidone 2.0%, isolation layer film-forming material hypromellose 13.9%, disintegrant B crospovidone 6.9% and Solvent A sodium lauryl sulfate 2.3%;

[0090] Relative to the delayed-release part in the zaleplon double-release capsule, the delayed-release pellets are made up of the following raw materials in percentage by weight: zaleplon 14.3%, sucrose pell...

Embodiment 2

[0092] The preparation method of the above-mentioned embodiment 1 zaleplon double-release capsules, its detailed steps are as follows:

[0093] Firstly, the drug-loaded pellet cores are prepared according to the drug formula, and the immediate-release pellets are prepared from the drug-loaded pellet cores, and then the delayed-release pellets are prepared from the immediate-release pellets, and finally the prepared immediate-release pellets and delayed-release pellets are respectively filled into capsules to obtain Zhalai Pron double release capsules;

[0094] (1) Preparation of drug-loaded pellet core:

[0095] The composition of the drug-loaded pill core: Zaleplon 92.4g, sucrose pellets (30-40 mesh) 210g, filler mannitol 80.85g, binder hypromellose 46.2g, disintegrant A cross-linked polymer Vitone 11.55g, 10% ethanol aqueous solution 924g (the ethanol aqueous solution is used as a solvent, and the solvent evaporates after this process);

[0096] Preparation process: first,...

Embodiment 3

[0110] Zaleplon double-release capsules of the present invention comprise quick-release pellets and delayed-release pellets, and the weight percentages of the quick-release pellets and delayed-release pellets are respectively 40% and 60%, i.e. immediate release The mass ratio between the pellets and the delayed-release pellets is 2:3;

[0111]With respect to the immediate-release part in the zaleplon double-release capsules, the quick-release pellets are made up of the following raw materials in percentage by weight: zaleplon 19.1%, sucrose pellets 43.3%, filler mannitol 16.7% , binder hypromellose 9.5%, disintegrant A crospovidone 2.4%, isolation layer film-forming material Opadry 9.0%;

[0112] Relative to the delayed-release part in the zaleplon double-release capsule, the delayed-release pellets are made up of the following raw materials in percentage by weight: zaleplon 14.7%, sucrose pellets 33.3%, filler mannitol 12.8% , binder hypromellose 7.3%, disintegrant A crospov...

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Abstract

The invention discloses a zaleplon double-release capsule and a preparation method thereof. The zaleplon double-release capsule comprises quick-release pellets and slow-release pellets, wherein each quick-release pellet consists of zaleplon, blank pellet, filler, an adhesive, a disintegrating agent A, an isolation layer film forming material, 0 to 8 percent of a disintegrating agent B and a solubilizer A; and each slow-release pellet comprises zaleplon, blank pellet, filler, an adhesive, the disintegrating agent A, the isolation layer film forming material, the disintegrating agent B, the solubilizer A, a slow-release material, a plasticizer, an antisticking agent and a solubilizer B. The preparation method comprises the following steps: preparing a pellet carrying core; preparing quick-release pellets by the pellet carrying core; preparing slow-release pellets by the quick-release pellets; and filling the quick-release pellets and the slow-release pellets into capsules respectively to obtain the zaleplon double-release capsules. Used for treating insomnia, the zaleplon double-release capsules prepared by the method can increase sleeping period and reduce the number of wakening, so that the treatment effect to a patient can be improved.

Description

technical field [0001] The invention relates to a preparation method of pharmaceutical preparations in the pharmaceutical field, in particular to a zaleplon double-release capsule preparation and a preparation method thereof. Background technique [0002] In the early days, the treatment of insomnia usually used central nervous system drugs barbiturates and benzodiazepine sedatives, but they have recognized side effects, such as drowsiness, depression, addiction, etc. Recently, the treatment of insomnia has begun to use non-benzodiazepines, Ambien TM (zolpidem) and Sonata TM (zaleplon) is an example of an approved drug product. Despite the great advancements in available APIs, the inherent properties of such APIs, such as short half-lives, will largely affect their effectiveness, side effect profile, and patient acceptance. Immediate-release dosage forms of this class of drugs are usually effective, providing rapid release of the drug shortly after ingestion, causing rapi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/519A61K47/38A61P25/20
Inventor 王军任逢晓
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD
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